Piret Jocelyne, Laforest Geneviève, Bussières Martin, Bergeron Michel G
Centre de recherche en infectiologie, Laval University, Quebec, Quebec, Canada, G1V 4G2.
J Appl Toxicol. 2008 Mar;28(2):164-74. doi: 10.1002/jat.1262.
The safety of an ethylene oxide/propylene oxide gel formulation containing sodium lauryl sulfate (2%, w/w), that could be a potent candidate as a topical microbicide, has been evaluated. More specifically, the subchronic (26- and 52-week) toxicity of the formulation when applied intravaginally as well as its irritating potential for the rectal, penile, eye, skin and buccal mucosa have been examined in animal models. The results showed that the vaginal administration of the gel formulation containing sodium lauryl sulfate once and twice daily (with doses 12 +/- 2 h apart) for 26 weeks to rats and for 52 weeks to rabbits induced slight to moderate histopathological alterations. When the formulation was applied intrarectally to male and female rabbits once and twice daily (with doses 12 +/- 2 h apart) for 14 days, no macroscopic or microscopic changes were reported. For both vaginal and rectal dosing, no effect was seen on the haematology, coagulation and serum chemistry parameters as well as on the body weight of animals and the relative organ weights. Other sporadic macroscopic and histopathological findings were incidental in origin and of no toxicological significance. The gel formulation containing sodium lauryl sulfate was considered as mildly irritating for the penile mucosa of rabbits, non-irritating for the eye of rabbits, mildly irritating for the skin in a rabbit model and non-irritating for the hamster cheek pouch. It is suggested that the gel formulation containing sodium lauryl sulfate is safe for most tissues that could be exposed to the product under normal use.
一种含有月桂醇硫酸酯钠（2%，w/w）的环氧乙烷/环氧丙烷凝胶制剂，有望成为一种有效的局部杀菌剂，其安全性已得到评估。更具体地说，已在动物模型中研究了该制剂经阴道给药时的亚慢性（26周和52周）毒性，以及其对直肠、阴茎、眼睛、皮肤和口腔黏膜的刺激潜力。结果表明，每天一次和两次（剂量间隔12±2小时）给大鼠阴道给药含月桂醇硫酸酯钠的凝胶制剂26周，给兔子阴道给药52周，会引起轻微至中度的组织病理学改变。当该制剂每天一次和两次（剂量间隔12±2小时）经直肠给雄性和雌性兔子给药14天时，未报告有肉眼或显微镜下的变化。对于阴道和直肠给药，在血液学、凝血和血清化学参数以及动物体重和相对器官重量方面均未观察到影响。其他偶发的肉眼和组织病理学发现为偶然发生，无毒理学意义。含月桂醇硫酸酯钠的凝胶制剂对兔子阴茎黏膜有轻度刺激，对兔子眼睛无刺激，在兔子模型中对皮肤有轻度刺激，对仓鼠颊囊无刺激。建议含月桂醇硫酸酯钠的凝胶制剂对正常使用情况下可能接触该产品的大多数组织是安全的。
